CAS: 368421-58-3; (2R,3R)-3-(2,5-Difluorophenyl)-3-Hydroxy-2-Methyl-4-(1H-1,2,4-Triazol-1-yl)Thiobutyramide

上下游产品

艾沙康唑中间体6 (2R,3R)-3-(2,5-Difluorophenyl)-3-Hydroxy-2-Methyl-4-(1H-1,2,4-Triazol-1-yl)Butanamide 241479-75-4
艾沙康唑中间体7 (2S,3R)-3-(2,5-Difluorophenyl)-3-Hydroxy-2-Methyl-4-(1H-1,2,4-Triazol-1-yl)Butanenitrile 241479-74-3
3-(2,5-Difluorophenyl)-3-Hydroxy-2-Methyl-4-(1H-1,2,4-Triazol-1-yl) Butyronitrile
1-[[(2R,3S)-2-(2,5-二氟苯基)-3-甲基环氧乙烷基]甲基]-1H-1,2,4-三唑 (2R,3S)-2-(2,5-Difluorophenyl)-3-Methyl-2-[(1H-1,2,4-Triazol-1-yl)-Methyl]-Oxirane 241479-73-2

2,5-二氟苯胺置于哌啶,三氟化硼乙醚,四丁基氟化铵,C37H56N4O4,Potassium Carbonate,溶剂黄146,甲基磺酰氯,二硫代磷酸二乙酯,三乙胺,Cobalt(II) Chloride,Scandium Tris(Trifluoromethanesulfonate)体系中,用 四氢呋喃,甲醇,二氯甲烷,水,异丙醇,乙腈 用作溶剂,化学反应 107.49H,反应生成(2R,3R)-3-(2,5-二氟苯基)-3-羟基-2-甲基-4-[1H-(1,2,4)-三氮唑-1-基]硫代丁酰胺
参考文献:末端烯酮的不对称催化环氧化合成三唑类抗真菌剂
标题:末端烯酮的不对称催化环氧化合成三唑类抗真菌剂
摘要:实现了α-取代乙烯基酮的对映选择性环氧化,构建了合成各种三唑类抗真菌剂的关键环氧化物中间体.通过使用手性n,N'-二氧化物/sc Iii配合物作为手性催化剂和 35% 的水溶液,该反应以高产率和非常好的对映选择性有效进行.H 2 O 2作为氧化剂.它使光学活性艾沙康唑,依氟康唑和其他潜在的抗真菌剂的转化成为可能.
Doi:10.1021/acs.Orglett.1C02588

专利信息

专利号:WO-2023237534-A1
优先权日:2022-06-07
标 题:A process for preparing isavuconazonium sulfate
发明人：HALUSZCZUK ADAM ANDRZEJ; KOSIK KAMIL; GRAUZENIS MACIEJ; BRODA EWA
权利人:ZAKL FARMACEUTYCZNE POLPHARMA S A
摘要:The present invention relates to a process for preparing isavuconazonium sulfate and a process for isolation and/or purification of isavuconazonium sulfate. Further, the invention relates to new isavuconazonium salts useful in the preparation and/or purification of isavuconazonium sulfate and a process for their preparation. Additionally, the invention provides a new intermediate useful in the synthesis of isavuconazonium.